Geneva Pharmaceuticals, Inc.

Sandoz Ag

Sandoz Gmbh

Hiren V Patel

Mahendra R Patel

Anup Kumar Ray

Shilpa V Merai

Johannes Ludescher

Ingolf Macher

Mariappan Anbazhagan

Pramod B Patel

The present invention relates to an improved process for preparing a polypeptide or pharmaceutically acceptable salt thereof comprising L-tyrosine, L-alanine, L-glutamate, and L-lysine. The polypeptide or pharmaceutically acceptable salt thereof is preferably glatiramer acetate. The process comprises: (a) polymerizing a mixture of N-carboxyanhydride of L-tyrosine, N-carboxyanhydride of L-alanine, N-carboxyanhydride of a protected L-glutamate and N-carboxyanhydride of a protected L-lysine, in a polar aprotic solvent in the presence of an initiator, to form a protected polypeptide; (b) admixing an acid with the protected polypeptide formed in Step (a) and a solvent, to form a product; and (c) admixing a substance selected from the group consisting of an alkali or alkaline earth metal hydroxide, a carbonate, a hydrogencarbonate, and mixtures thereof, with the product formed in Step (b), and a solvent or a mixture of a solvent and water, to form a deprotected polypeptide or a pharmaceutically acceptable salt thereof.

Processes for preparing a polypeptide

A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine, or olanzapine.

Process of preparation of olanzapine form I

This invention provides a process of preparation of novel polymorphic hemifumarate salts of 8-chloro-6,11-dihyfro-11-(4-piperidylidene)-5H-benzo[5,6]-cyclohepta[1,2-b]pyridine, hereinafter called 'desloratadine'. These polymorphic salt forms show much higher solubility in water and also in protic organic solvents compare to the parent desloratadine. The process of preparing the polymorphic forms comprising:

Salt and polymorphs of desloratadine hemifumarate

This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.

&agr;, &agr;-dibromo-&agr;-chloro-acetophenones as synthons

&agr;,&agr;-dibromo-&agr;-chloro-acetophenones as synthons

Midodrine hydrochloride, &plusmn;1-(2&prime;,5&prime;-dimethoxyphenyl)-2-glycineamido-ethanol-(1)-HCl, is prepared from a novel intermediate, 1-(2&prime;,5&prime;-dimethoxyphenyl)-2-azidoethanone.

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Hiren V Patel